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Drug complexes for preventing and curing schemic cerebrovaseular disease as well as preparation method thereof

A technology for cerebrovascular disease and ischemia, which is applied in the field of drug compound and its preparation for the prevention and treatment of ischemic cerebrovascular disease, and can solve the problems such as poor curative effect of ischemic cerebrovascular disease

Inactive Publication Date: 2008-05-21
SUN YAT SEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The purpose of the present invention is to overcome the disadvantages of poor curative effect of the existing single use of ferulic acid and borneol in the treatment of ischemic cerebrovascular diseases, and to provide a drug with synergistic and complementary pharmacological effects, fast onset, prolonged effective time, and small dosage. A pharmaceutical composition for preventing and treating ischemic cerebrovascular disease with definite curative effect and its preparation method

Method used

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  • Drug complexes for preventing and curing schemic cerebrovaseular disease as well as preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Pharmacodynamics Example 1: Comparison of Postoperative Mortality and Epilepsy Rate in Transient Global Cerebral Ischemia Mice

[0046] Global cerebral ischemia can induce epilepsy. After operation, mice in each group were observed for death and whether epilepsy was induced. There are mainly four types of epileptic seizures: ① Running wildly: running continuously without changing direction, and not actively avoiding obstacles. The gallop may be accompanied by twitching of the whiskers and loud breathing. If the mouse is kept in a cage, it will hit the container wall or jump up and hit the cage lid. Stampede can last about 30s to 1min. ② generalized clonus: refers to body and limb clonus. ③Focal clonus: refers to localized head / forelimb or hindlimb / tail clonus. ④ Limb twitching: the mouse stands on its hind legs, its forelimbs twitch, and it can be seen that it loses balance.

[0047] Table 1 Comparison of 24h postoperative mortality and epilepsy rates in mice with...

Embodiment 2

[0051] Pharmacodynamics Example 2: Postoperative Neurological Function Score of Transient Global Cerebral Ischemia Mice

[0052] The neurological function scores of mice in each group were scored in the same environment after waking up from surgery (4-6 hours), 24 hours and 48 hours respectively. The Zea Longa 5-point scoring system was used: 0 points, no symptoms of nerve damage; 1 point, unable to stretch the forepaws; 2 points, turning to the outside; 3 points, falling to the outside; 4 points, unable to walk spontaneously, loss of consciousness, The higher the score, the more severe the animal's behavioral disturbance.

[0053] Table 2 Comparison of postoperative neurological function scores of mice with global cerebral ischemia in each group ( )

[0054]

group

After the animal wakes up (4~6h)

animal score

24h

48h

SAM (n=12)

VEH (n=11)

PIRACETAMUM (n=12)

PIRACETAMUM SAM (n=12)

SF100 (n=12)

...

Embodiment 3

[0058] Pharmacodynamics Example 3: Morris Water Maze Test on Transient Global Cerebral Ischemia Mice

[0059] It is mainly divided into concealed platform test and exploratory test. The circular pool of the water maze device has a diameter of 100 cm, a height of 40 cm, a water depth of 25 cm, and a water temperature of 22±0.5°C; a transparent circular platform with a diameter of 10 cm and a height of 24 cm is placed in the southwest quadrant and submerged 1 cm below the water surface, so that the mice can swim in the pool The platform below the surface cannot be seen from time to time. There were 12 mice in each group. On the 4th day after operation, the mice were put into the pool of the water maze device to swim freely for 90 seconds without placing a platform to exclude animals with swimming impairments. The concealed platform test was tested on the 5th day after the operation. Four times a day, the mice were put into the pool from the four quadrants facing the pool wall f...

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Abstract

The invention provides a pharmaceutical composition for the prevention and treatment of ischemic cerebrovascular diseases and the preparation method thereof, which contains active ingredients and carriers, wherein the active ingredients consist of fumalic acid or the pharmaceutically acceptable salt and borneol with the weight ratio of 100: 0.5 to 10. The invention can be prepared into the pharmaceutical formulations which are applicable to the clinical application, and the formulations include: granules, capsules, tablets, dropping pills, suppositories and injections. The invention reveals the neuro-protective effect of the composition of fumalic acid or the salt and borneol for transient total cerebral ischemia, and the synergy of the two drugs is played by the combination of the two; compared with single fumalic acid, the absorption half-life is prolonged, the time for reaching peak is faster, the dosage of fumalic acid is reduced and the safety of the drugs is increased. The invention has the advantages of the complementary and synergy of pharmacological effects, instant effects, prolonged effective time, small dosage and precise efficacy when being taken as the drug for the prevention and treatment of ischemic cerebrovascular diseases.

Description

【Technical field】 [0001] The invention relates to a pharmaceutical composition for preventing and treating ischemic cerebrovascular disease and a preparation method thereof. 【Background technique】 [0002] With the aging of the population in today's society, the incidence of cerebrovascular disease continues to increase. It has the characteristics of "three highs": high incidence, high disability, and high mortality. It has become one of the major diseases that seriously endanger human health. Among the 57 countries surveyed by the United Nations WHO, cerebrovascular diseases accounted for 11.3% of deaths, among which cerebrovascular diseases accounted for the top three causes of death in 40 countries. The total number of stroke patients in the United States is more than 4 million. About 1 million people die from cerebrovascular disease in my country every year. In 2003, cerebrovascular disease ranked second among the causes of death in both urban and rural areas, second on...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/192A61P9/10A61K31/045
Inventor 皮荣标林竹贞姚美村刘培庆
Owner SUN YAT SEN UNIV
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